3-(2-Hydroxyethyl)-1-[3-methoxy-4-(2-pyrrolidin-1-ylethoxy)phenyl]pyrazin-2-one | 942910-41-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-(2-Hydroxyethyl)-1-[3-methoxy-4-(2-pyrrolidin-1-ylethoxy)phenyl]pyrazin-2-one
• CAS: 942910-41-0
• 化学式: C₁₉H₂₅N₃O₄
• 分子量: 359.425
• InChiKey: DYIINYHMPFAPNC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  74.6
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  3-(2-Hydroxyethyl)-1-[3-methoxy-4-(2-pyrrolidin-1-ylethoxy)phenyl]pyrazin-2-one 、 苯基三氟硼酸钾 在 4-二甲氨基吡啶 、 copper diacetate 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 以6%的产率得到1-[3-Methoxy-4-(2-pyrrolidin-1-ylethoxy)phenyl]-3-(2-phenoxyethyl)pyrazin-2-one
  参考文献：
  名称：

  WO2007/71646

  摘要：

  公开号：
• 作为产物：
  描述：

  4-bromo-2-methoxyphenyl-2-(1-pyrrolidinyl)ethyl ether 、 3-(2-hydroxyethyl)-1H-pyrazin-2-one 在 potassium phosphate 、 copper(l) iodide 、 N,N'-二甲基乙二胺 作用下， 以 1,4-二氧六环 、 N,N-二甲基甲酰胺 为溶剂， 反应 0.5h， 以30%的产率得到3-(2-Hydroxyethyl)-1-[3-methoxy-4-(2-pyrrolidin-1-ylethoxy)phenyl]pyrazin-2-one
  参考文献：
  名称：

  WO2007/71646

  摘要：

  公开号：

文献信息

• NOVEL SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE IN MCH-1 MEDIATED DISEASES
  申请人：Janssen Pharmaceutica N.V.

  公开号：EP1966164B1

  公开（公告）日：2013-03-06
• Novel Substituted Pyrazinone Derivatives for Use in Mch-1 Mediated Diseases
  申请人：Andres-Gil Jose Ignacio

  公开号：US20090012062A1

  公开（公告）日：2009-01-08

  The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1 . It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.
• US8329704B2
  申请人：——

  公开号：US8329704B2

  公开（公告）日：2012-12-11
• [EN] NOVEL SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE IN MCH-1 MEDIATED DISEASES<br/>[FR] NOUVEAUX DERIVES DE PYRAZINONE SUBSTITUEE A UTILISER LORS DE MALADIES MEDIEES PAR MCH-1
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2007071646A1

  公开（公告）日：2007-06-28

  [EN] The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-I activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereo chemically isomeric form thereof, an TV-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders ; obesity ; diabetes ; sexual disorders and neurological disorders.
  [FR] L'invention concerne des dérivés de pyrazinone substituée par aryle et hétéroaryle présentant une activité d'hormone de concentration en mélanine (MCH) antagoniste, en particulier une activité de MCH-1 selon la formule générale (I), un sel d'addition d'acide ou de base, une forme stéréo-chimiquement isomère, une forme deN-oxyde ou un sel d'ammonium quaternaire de ceux-ci pharmaceutiquement acceptable, dont les paramètres sont définis dans la Revendication 1. L'invention concerne en outre la préparation de ces dérivés, les compositions les renfermant et leur utilisation comme médicament. Les composés selon l'invention servent à prévenir et/ou à traiter des troubles psychiatriques, notamment l'anxiété, les troubles de l'alimentation, les troubles de l'humeur, par exemple les troubles bipolaires et la dépression, les psychoses, par exemple la schizophrénie, et les troubles du sommeil; l'obésité; les diabètes; les troubles sexuels et les troubles neurologiques.